13C-labelling of the side-chains in Mitoxantrone

The antineoplastic drug, mitoxantrone (5,8-Bis-{[1-13C]-{[2-[2-hydroxyethyl)amino]ethyl]amino}}-1,4-di-(hydroxcy-9,10-anthracenedione dihydrochloride) is synthesized in 28% yield from [13C]-sodium cyanide via a five step sequence. The described synthesis of the sidechain, 2-[(2-aminoethyl)amino]ethanol, allows the labelling of each position of the carbon skeleton by taking use of only one intermediate, which is easy to prepare in very good yield. (author)